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vandetanib + selumetinib
- Development stage
- Phase 1
- Lead developer
- AstraZeneca
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules
- Administration
- Oral
01
Overview
Vandetanib + selumetinib is an investigational oral combination therapy of two small molecule inhibitors developed for the treatment of solid tumors, including non-small cell lung cancer (NSCLC). Vandetanib is a tyrosine kinase inhibitor that targets vascular endothelial growth factor receptor (VEGFR), epidermal growth factor receptor (EGFR), and RET tyrosine kinases. Selumetinib is a MEK inhibitor targeting the mitogen-activated protein kinase pathway. The rationale for combining these agents is to simultaneously inhibit multiple signaling pathways involved in tumor cell proliferation and survival. Phase I studies have shown that the combination can be administered with manageable toxicity, with dose-limiting toxicities primarily related to known side effects of each agent. The combination has demonstrated stable disease in some NSCLC patients but further efficacy data are limited[1][2][3][4][5].
- Other names
- VanSel-1VanSel1VanSel 1
02
Targets
PTK6 (Protein-tyrosine kinase 6)EGFR (Epidermal growth factor receptor)KCNH2 (Voltage-gated potassium channel subfamily H member 2)MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)MEK2 (Dual specificity mitogen-activated protein kinase kinase 2)RET (Rearranged during transfection receptor tyrosine kinase)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR4 (Vascular endothelial growth factor Receptor-3)
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